Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides are potent antagonists of the human H3-receptor

Bernd Peschke; Sonja Bak; Rolf Hohlweg; Rita Nielsen; Dorthe Viuff; Karin Rimvall

doi:10.1016/j.bmcl.2006.03.074

Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides are potent antagonists of the human H3-receptor

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3162-5. doi: 10.1016/j.bmcl.2006.03.074. Epub 2006 Apr 17.

Authors

Bernd Peschke¹, Sonja Bak, Rolf Hohlweg, Rita Nielsen, Dorthe Viuff, Karin Rimvall

Affiliation

¹ Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Maaloev, Denmark. bpes@novonordisk.com

PMID: 16616493
DOI: 10.1016/j.bmcl.2006.03.074

Abstract

Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides have been found to be antagonists on the human histamine-3-receptor, showing a Ki value of as low as 4 nM.

MeSH terms

Amides / chemical synthesis
Amides / chemistry*
Amides / pharmacology*
Benzene / chemistry
Furans / chemistry*
Histamine Antagonists / chemical synthesis*
Histamine Antagonists / chemistry
Histamine Antagonists / pharmacology*
Humans
Molecular Structure
Receptors, Histamine H3 / metabolism*
Structure-Activity Relationship
Thiophenes / chemistry*

Substances

Amides
Furans
Histamine Antagonists
Receptors, Histamine H3
Thiophenes
Benzene
furan